Target intelligence / Profile preview

GABA Transporters (GATs)

Target
GATs
Molecular classification
Transporter, Solute carrier family 6 (SLC6), Sodium-dependent transporters, Chloride-dependent transporters
01

Overview

GABA transporters (GATs) are membrane proteins responsible for the reuptake of GABA, the primary inhibitory neurotransmitter in the mammalian central nervous system. They play a crucial role in regulating extracellular GABA concentrations, thereby controlling synaptic transmission and maintaining neural circuit balance. There are four main plasma membrane GABA transporter subtypes: GAT1 (SLC6A1), GAT2 (SLC6A13), GAT3 (SLC6A11), and BGT1 (SLC6A12). These transporters clear released GABA from the synaptic cleft, terminating inhibitory signaling and maintaining homeostasis. Dysfunction or reversal of GAT function can contribute to neurological disorders like epilepsy. Inhibitors targeting these transporters, such as tiagabine, are used to modulate inhibition.

Other names
GABA uptake transportersgamma-aminobutyric acid transportersSLC6A1SLC6A13SLC6A11SLC6A12
02

Mechanism of action

Inhibition of GABA reuptake, increasing extracellular GABA concentration.

03

Biological functions

Neurotransmitter reuptakeRegulation of synaptic transmissionRegulation of extracellular GABA concentrationTermination of inhibitory signalingMaintenance of neural circuit balanceHomeostasis of inhibitory tone
04

Disease associations

EpilepsySeizure disordersNeurological disorders
05

Safety considerations

Potential for altered inhibition leading to pathological statesDysregulation can increase seizure susceptibility
06

Interacting drugs

Tiagabine

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